Plasma stability and cytotoxicity of lipophilic daunorubicin derivatives incorporated into low density lipoproteins

Michèle Masquelier, Gunars Tirzitis, Curt O. Peterson, Magdalena Pålsson, Andris Amolins, Mara Plotniece, Aiva Plotniece, Natalja Makarova, Sigurd G. Vitols

Research output: Contribution to journalArticlepeer-review

4 Citations (Scopus)


The selective targeting of antineoplastic drugs to tumours by incorporation in low density lipoproteins (LDL) is an attractive possibility if the drug-LDL complex remains stable in the circulation and is taken up by the tumour. In previous studies we have shown that vincristine- and N- trifluoroacetyladriamycin-14-valerate-LDL complexes were unstable in vivo. We synthesized five N-substituted lipophilic derivatives of daunorubicin and studied their incorporation into LDL. Three out of five daunorubicin derivatives incorporated successfully into LDL. In vitro these complexes were more cytotoxic towards LDL receptor positive Chinese hamster ovary cells than LDL receptor negative cells. Non-specific cytotoxicity was explained by slow dissociation of the drug-LDL complex in plasma. Our results underline the importance of careful studies of plasma stability when investigating lipoproteins and other carriers in drug targeting. (C) 2000 Editions scientifiques et medicales Elsevier SAS.

Original languageEnglish
Pages (from-to)429-438
Number of pages10
JournalEuropean Journal of Medicinal Chemistry
Issue number4
Publication statusPublished - Apr 2000
Externally publishedYes


  • Daunorubicin derivatives
  • Drug carrier
  • Low-density lipoprotein
  • Tumour therapy

Field of Science*

  • 1.4 Chemical sciences
  • 3.1 Basic medicine

Publication Type*

  • 1.1. Scientific article indexed in Web of Science and/or Scopus database


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